Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease
Increasingly attention has been paid to the transdermal drug delivery systems with microneedles owing to their excellent compliance, high efficiency, and controllable drug release, therefore, become promising alternative with tremendous advantages for delivering specific drugs such as huperzine A (H...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2020-01-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2020.1797240 |
| _version_ | 1818924580322934784 |
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| author | Qinying Yan Weiwei Wang Jiaqi Weng Zhenghan Zhang Lina Yin Qingliang Yang Fangyuan Guo Xingang Wang Fan Chen Gensheng Yang |
| author_facet | Qinying Yan Weiwei Wang Jiaqi Weng Zhenghan Zhang Lina Yin Qingliang Yang Fangyuan Guo Xingang Wang Fan Chen Gensheng Yang |
| author_sort | Qinying Yan |
| collection | DOAJ |
| description | Increasingly attention has been paid to the transdermal drug delivery systems with microneedles owing to their excellent compliance, high efficiency, and controllable drug release, therefore, become promising alternative with tremendous advantages for delivering specific drugs such as huperzine A (Hup A) for treatment of Alzheimer’s disease (AD) yet with low oral bioavailability. The purpose of the present study is to design, prepare, and evaluate a dissolving microneedle patch (DMNP) as a transdermal delivery system for the Hup A, investigating its in vitro drug release profiles and in vivo pharmacokinetics as well as pharmacodynamics treating of AD. Skin penetration experiments and intradermal dissolution tests showed that the blank DMNP could successfully penetrate the skin with an adequate depth and could be quickly dissolved within 5 min. In vitro transdermal release tests exhibited that more than 80% of the Hup A was accumulatively permeated from DMNP through the skin within three days, indicating a sustained release profile. In vivo pharmacokinetic analysis demonstrated that the DMNP group resulted in longer Tmax (twofold), longer t1/2 (fivefold), lower Cmax (3:4), and larger AUC(0–∞) (twofold), compared with the oral group at the same dose of Hup A. Pharmacodynamic research showed a significant improvement in cognitive function in AD rats treated with DMNP-Hup A and Oral-Hup A, as compared to the model group without treatment. Those results demonstrated that this predesigned DMNP is a promising alternative to deliver Hup A transdermally for the treatment of AD. |
| first_indexed | 2024-12-20T02:27:35Z |
| format | Article |
| id | doaj.art-1f4a1cd0f7fe44f28b0ef87664460c77 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-20T02:27:35Z |
| publishDate | 2020-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-1f4a1cd0f7fe44f28b0ef87664460c772022-12-21T19:56:39ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642020-01-012711147115510.1080/10717544.2020.17972401797240Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's diseaseQinying Yan0Weiwei Wang1Jiaqi Weng2Zhenghan Zhang3Lina Yin4Qingliang Yang5Fangyuan Guo6Xingang Wang7Fan Chen8Gensheng Yang9College of Pharmaceutical Sciences, Zhejiang University of TechnologyCollege of Pharmaceutical Sciences, Zhejiang University of TechnologyCollege of Pharmaceutical Sciences, Zhejiang University of TechnologyCollege of Pharmaceutical Sciences, Zhejiang University of TechnologyZhejiang Academy of Medical Sciences, Institute of Materia MedicaCollege of Pharmaceutical Sciences, Zhejiang University of TechnologyCollege of Pharmaceutical Sciences, Zhejiang University of TechnologyDepartment of Burns, School of Medicine, Second Affiliated Hospital of Zhejiang UniversityHubei Collaborative Innovation Center for Green Transformation of Bio-Resources, Life Sciences School of Hubei UniversityCollege of Pharmaceutical Sciences, Zhejiang University of TechnologyIncreasingly attention has been paid to the transdermal drug delivery systems with microneedles owing to their excellent compliance, high efficiency, and controllable drug release, therefore, become promising alternative with tremendous advantages for delivering specific drugs such as huperzine A (Hup A) for treatment of Alzheimer’s disease (AD) yet with low oral bioavailability. The purpose of the present study is to design, prepare, and evaluate a dissolving microneedle patch (DMNP) as a transdermal delivery system for the Hup A, investigating its in vitro drug release profiles and in vivo pharmacokinetics as well as pharmacodynamics treating of AD. Skin penetration experiments and intradermal dissolution tests showed that the blank DMNP could successfully penetrate the skin with an adequate depth and could be quickly dissolved within 5 min. In vitro transdermal release tests exhibited that more than 80% of the Hup A was accumulatively permeated from DMNP through the skin within three days, indicating a sustained release profile. In vivo pharmacokinetic analysis demonstrated that the DMNP group resulted in longer Tmax (twofold), longer t1/2 (fivefold), lower Cmax (3:4), and larger AUC(0–∞) (twofold), compared with the oral group at the same dose of Hup A. Pharmacodynamic research showed a significant improvement in cognitive function in AD rats treated with DMNP-Hup A and Oral-Hup A, as compared to the model group without treatment. Those results demonstrated that this predesigned DMNP is a promising alternative to deliver Hup A transdermally for the treatment of AD.http://dx.doi.org/10.1080/10717544.2020.1797240dissolving microneedlestransdermal deliveryhuperzine aalzheimer's disease |
| spellingShingle | Qinying Yan Weiwei Wang Jiaqi Weng Zhenghan Zhang Lina Yin Qingliang Yang Fangyuan Guo Xingang Wang Fan Chen Gensheng Yang Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease Drug Delivery dissolving microneedles transdermal delivery huperzine a alzheimer's disease |
| title | Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease |
| title_full | Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease |
| title_fullStr | Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease |
| title_full_unstemmed | Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease |
| title_short | Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease |
| title_sort | dissolving microneedles for transdermal delivery of huperzine a for the treatment of alzheimer s disease |
| topic | dissolving microneedles transdermal delivery huperzine a alzheimer's disease |
| url | http://dx.doi.org/10.1080/10717544.2020.1797240 |
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